Discovery of 1,4-pentadien-3-one derivatives containing quinoxaline scaffolds as potential apoptosis inducers
Aim: To synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities against SMMC-7721 cells in vitro compared with the well-known antitumor drug gemcitabine. The mechanistic investigation showed that compounds N3 and N4 induced SMMC-7721 cell apoptosis by regulating the expression levels of apoptosis-related proteins. In addition, the molecular docking model further revealed that compound N3 could be a potential peroxisome proliferator-activated receptor inhibitor. Conclusion: These compounds might serve as bioactive fragments and lead compounds for developing more potent apoptosis inducers.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Future medicinal chemistry - 12(2020), 16 vom: 28. Aug., Seite 1505-1519 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Tang, Xu [VerfasserIn] |
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| Links: |
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| Themen: |
1,4-pentadien-3-one |
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| Anmerkungen: |
Date Completed 14.07.2021 Date Revised 14.07.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2019-0371 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM313476853 |
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| 245 | 1 | 0 | |a Discovery of 1,4-pentadien-3-one derivatives containing quinoxaline scaffolds as potential apoptosis inducers |
| 264 | 1 | |c 2020 | |
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| 500 | |a Date Completed 14.07.2021 | ||
| 500 | |a Date Revised 14.07.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: To synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities against SMMC-7721 cells in vitro compared with the well-known antitumor drug gemcitabine. The mechanistic investigation showed that compounds N3 and N4 induced SMMC-7721 cell apoptosis by regulating the expression levels of apoptosis-related proteins. In addition, the molecular docking model further revealed that compound N3 could be a potential peroxisome proliferator-activated receptor inhibitor. Conclusion: These compounds might serve as bioactive fragments and lead compounds for developing more potent apoptosis inducers | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a 1,4-pentadien-3-one | |
| 650 | 4 | |a SMMC-7721 cells | |
| 650 | 4 | |a antiproliferative activities | |
| 650 | 4 | |a quinoxaline | |
| 650 | 7 | |a Alkadienes |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Quinoxalines |2 NLM | |
| 700 | 1 | |a He, Jun |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Qin |e verfasserin |4 aut | |
| 700 | 1 | |a Tang, Xuemei |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Mei |e verfasserin |4 aut | |
| 700 | 1 | |a Hao, Gefei |e verfasserin |4 aut | |
| 700 | 1 | |a Huai, Ziyou |e verfasserin |4 aut | |
| 700 | 1 | |a Huang, Yinjin |e verfasserin |4 aut | |
| 700 | 1 | |a Xue, Wei |e verfasserin |4 aut | |
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